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NBI-42902 manufacturers
- NBI-42902
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- $1710.00
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2026-05-11
- CAS:352290-60-9
- Purity:
- Supply Ability: 10g
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| | NBI-42902 Basic information |
| Product Name: | NBI-42902 | | Synonyms: | NBI-42902;3-[(2R)-2-Amino-2-phenylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyl-2,4(1H,3H)-pyrimidinedione;CS-1113;NBI-42902;NBI 42902;2,4(1H,3H)-Pyrimidinedione, 3-[(2R)-2-amino-2-phenylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyl-;(R)-3-(2-amino-2-phenylethyl)-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4(1H,3H)-dione | | CAS: | 352290-60-9 | | MF: | C27H24F3N3O3 | | MW: | 495.49 | | EINECS: | | | Product Categories: | | | Mol File: | 352290-60-9.mol |  |
| | NBI-42902 Chemical Properties |
| form | Solid | | color | White to off-white |
| | NBI-42902 Usage And Synthesis |
| Uses | NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases[1]. | | in vivo | NBI-42902 (10-100 mg/kg, p.o. or i.v. ) inhibits serum LH levels significantly in castrated macaques[1]. | Animal Model: | Castrated macaques[1] | | Dosage: | 10, 40, 100 mg/kg | | Administration: | Oral administration (p.o.) | | Result: | Inhibited serum LH with dose dependent.
Inhibited serum LH achieved maximum suppression, that was 62-68% of pretreatment baseline, at 4-8 h after administration.
Exhibited no suppression of LH levels after 24 h treated with 10 or 40 mg/kg, but remained suppression at 100 mg/kg.
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| Animal Model: | Castrated macaques[1] | | Dosage: | 10 mg/kg | | Administration: | Intravenous injection (i.v.) | | Result: | Inhibited serum LH achieved maximum suppression was 62-68% of pretreatment baseline between 4-8 h after administration, but exhibited no suppression after 24 h.
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| | References | [1] Struthers RS, et al. Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902. Endocrinology. 2007 Feb;148(2):857-67. DOI:10.1210/en.2006-1213 |
| | NBI-42902 Preparation Products And Raw materials |
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